公开(公告)号：US20210179560A1

公开(公告)日：2021-06-17

申请号：US16983027

申请日：2020-08-03

Applicant: Amgen Inc.

Inventor： Michael D. Bartberger ,  Ana Gonzalez Buenrostro ,  Hilary Plake Beck ,  Xiaoqi Chen ,  Richard Victor Connors ,  Jeffrey Deignan ,  Jason A. Duquette, I ,  John Eksterowicz ,  Benjamin Fisher ,  Brian M. Fox ,  Jiasheng Fu ,  Zice Fu ,  Felix Gonzalez Lopez De Turiso ,  Michael W. Gribble ,  Darin J. Gustin ,  Julie A. Heath ,  Xin Huang ,  XianYun Jiao ,  Michael G. Johnson ,  Frank Kayser ,  David John Kopecky ,  SuJen Lai ,  Yihong Li ,  Zhihong Li ,  Jiwen Liu ,  Jonathan D. Low ,  Brian S. Lucas ,  Zhihua MA ,  Lawrence R. McGee ,  Joel McIntosh ,  Dustin L. McMinn ,  Julio C. Medina ,  Jeffrey Thomas Mihalic ,  Steven H. Olson ,  Yossup Rew ,  Philip M. Roveto ,  Daqing Sun ,  Xiaodong Wang ,  Yingcai Wang ,  Xuelei Yan ,  Ming Yu ,  Jiang Zhu

IPC: C07D211/76 ,  C07D401/12 ,  C07D498/14 ,  C07D409/04 ,  C07D407/04 ,  C07D471/10 ,  C07D401/06 ,  C07D279/02 ,  C07D405/04 ,  C07D417/12 ,  C07D405/12 ,  C07D417/06 ,  C07D221/20 ,  C07D498/08 ,  C07D491/153 ,  C07D498/20 ,  C07D409/12 ,  C07D491/08 ,  C07D417/14 ,  C07D413/06 ,  C07D407/06 ,  C07D401/04

Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.

公开(公告)号：US09801867B2

公开(公告)日：2017-10-31

申请号：US15175824

申请日：2016-06-07

Applicant: AMGEN INC.

Inventor： Matthew Bio ,  Sebastien Caille ,  Brian Cochran ,  Yuanqing Fang ,  Brian M. Fox ,  Brian S. Lucas ,  Lawrence R. McGee ,  Filisaty Vounatsos ,  Sean H. Wiedemann ,  Sarah Wortman

IPC: C07D211/76 ,  A61K31/451 ,  C07D211/94 ,  C07D491/048 ,  C07C309/25 ,  C07C309/04 ,  C07C313/02 ,  C07D498/04 ,  C07C309/35

CPC classification number: A61K31/451 ,  C07B2200/13 ,  C07C309/04 ,  C07C309/25 ,  C07C309/35 ,  C07C313/02 ,  C07D211/76 ,  C07D211/94 ,  C07D491/048 ,  C07D498/04

Abstract: The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

公开(公告)号：US09623018B2

公开(公告)日：2017-04-18

申请号：US15175805

申请日：2016-06-07

Applicant: AMGEN INC.

Inventor： Matthew Bio ,  Sebastien Caille ,  Yuanqing Fang ,  Brian M. Fox ,  Brian S. Lucas ,  Lawrence R. McGee ,  Sean H. Wiedemann

IPC: C07D498/04 ,  A61K31/451 ,  C07D211/94 ,  C07D491/048 ,  C07C309/25 ,  C07C309/04 ,  C07D211/76 ,  C07C309/35

CPC classification number: A61K31/451 ,  C07B2200/13 ,  C07C309/04 ,  C07C309/25 ,  C07C309/35 ,  C07C313/02 ,  C07D211/76 ,  C07D211/94 ,  C07D491/048 ,  C07D498/04

Abstract: The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

公开(公告)号：US09376425B2

公开(公告)日：2016-06-28

申请号：US14347628

申请日：2012-09-26

Applicant: AMGEN INC.

Inventor： Michael D. Bartberger ,  Hilary Plake Beck ,  Xiaoqi Chen ,  Richard Victor Connors ,  Jeffrey Deignan ,  Jason A. Duquette ,  John Eksterowicz ,  Brian M. Fox ,  Jiasheng Fu ,  Ana Gonzalez Buenrostro ,  Felix Gonzalez Lopez De Turiso ,  Darin J. Gustin ,  Julie A. Heath ,  Michael G. Johnson ,  Frank Kayser ,  David John Kopecky ,  Yihong Li ,  Zhihong Li ,  Zhihua Ma ,  Joel McIntosh ,  Julio C. Medina ,  Jeffrey Thomas Mihalic ,  Steven H. Olson ,  Yosup Rew ,  Philip M. Roveto ,  Michael J. Schmitt ,  Daqing Sun ,  Xiaodong Wang ,  Malgorzata Wanska ,  Christine Weathers ,  Xuelei Yan

IPC: C07D265/06 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D413/12 ,  C07D265/32

CPC classification number: C07D413/04 ,  C07D265/06 ,  C07D265/32 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04

Abstract: The present invention provides MDM2 inhibitor compounds of Formula I or II, or the pharmaceutically acceptable salts thereof, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.

Abstract translation: 本发明提供式I或II的MDM2抑制剂化合物或其药学上可接受的盐，其中变量如上所定义，哪些化合物可用作治疗剂，特别是用于治疗癌症。 本发明还涉及含有MDM2抑制剂的药物组合物。